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Xanthone analogues as potent modulators of intestinal P-glycoprotein
- Xanthone analogues as potent modulators of intestinal P-glycoprotein
- Chae, Song Wha; Woo, Sangwook; Park, Jung Hyun; Kwon, Youngjoo; Na, Younghwa; Lee, Hwa Jeong
- Ewha Authors
- 이화정; 권영주
- SCOPUS Author ID
- 이화정; 권영주
- Issue Date
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- 0223-5234; 1768-3254
- vol. 93, pp. 237 - 245
- P-glycoprotein inhibitor; Xanthone analogue; Paclitaxel; Bioavailability; Xenograft
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- SCI; SCIE; SCOPUS
- Intestinal P-glycoprotein (P-gp) is a limiting step for oral absorption of drugs. Therefore, P-gp inhibitors have been studied as enhancers of oral absorption of drugs that are P-gp substrates. We investigated the in vitro and in vivo P-gp inhibitory activity of synthesized xanthone analogues. With 3-(3-chloro-2-hydroxypropoxy)-1-hydroxy-9H-thioxanthen-9-one, compound 13, accumulation of daunomycin (DNM) increased 707% and efflux of DNM decreased 66% compared to DNM alone. Relative bioavailability (RB) of paclitaxel (PTX, 25 mg/kg) increased 2.5-fold after oral administration with 13 (5 mg/kg). In a xenograft animal model, oral administration of PTX (40 mg/kg) with 13 (10 mg/kg) significantly inhibited tumour growth and was more effective than intravenously administered PTX (10 mg/kg) alone. Therefore, the synthesized xanthone analogue 13 might have therapeutic benefits for oral absorption of P-gp substrate anticancer drugs. (C) 2015 Published by Elsevier Masson SAS.
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